2-Aminotetralones: Novel inhibitors of MurA and MurZ

DUNSMORE, C. J., MILLER, K., BLAKE, K. L., PATCHING, S. G., HENDERSON, P. J. F., GARNETT, J. A., STUBBINGS, W. J., PHILLIPS, S. E. V., PALESTRANT, D. J. and ANGELES, J. de L. (2008). 2-Aminotetralones: Novel inhibitors of MurA and MurZ. Bioorganic & Medicinal Chemistry Letters, 18 (5), 1730-1734.

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Link to published version:: 10.1016/j.bmcl.2008.01.089

Abstract

Several 2-aminotetralones were identified as novel inhibitors of the bacterial enzymes MurA and MurZ. A number of these inhibitors demonstrated antibacterial activity against Staphylococcus aureus and Escherichia coli with MICs in the range 8-128 microg/ml. Based on structure-activity relationships we propose that the alpha-aminoketone functionality is responsible for the inhibitory activity and evidence is provided to support a covalent mode of action involving the C115 thiol group of MurA/MurZ.

Item Type: Article
Research Institute, Centre or Group: Biomedical Research Centre
Identification Number: 10.1016/j.bmcl.2008.01.089
Depositing User: Sarah Ward
Date Deposited: 28 Feb 2011 14:47
Last Modified: 28 Feb 2011 14:47
URI: http://shura.shu.ac.uk/id/eprint/3233

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